Bristol-myers Squibb Compnay

University of Connecticut

Chen Li

B Narasimhulu Naidu

Michael A Walker

Manoj Patel

Kevin M Peese

Nicholas A Meanwell

Alexandros Makriyannis

Yasutsugu Ueda

Timothy P Connolly

Margaret E Sorenson

Francis Beaulieu

Carl Ouellet

Andreas Goutopoulos

Annapurna Pendri

Jacques Banville

Katharine A Grant-Young

John D Matiskella

Michael S Bowsher

Roger Remillard

Barry L Johnson

Dai Lu

Ira B Dicker

Rongti Li

Yasutsuga Ueda

Jonathan R Weiss

Ting T Yin

The disclosure generally relates to the novel compounds of formula I, including their salts, which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV. 

HIV integrase inhibitors

One aspect of this disclosure relates generally to lipid compounds that exert diverse effects in the endocannabinoid system, such as regulating CB1 and CB2 receptor or moderating other bio-macromolecules within the endocannabinoid system. Some of the compounds showed improved receptor binding affinity, and/or improved receptor subtype selectivity, and improved bio-stability. Some of the compounds exhibit activities to regulate the enzymes that moderate the bio-disposal of endogenous cannabinoids, such as the fatty acid amide hydrolase (FAAH). Some of the compounds exhibit activities to inhibit the anandamide transporter. Other aspects of the invention are pharmaceutical preparations employing these ligands and methods of administering therapeutically effective amounts of the preparations to provide a physiological effect.

Cannabinergic lipid ligands

The invention encompasses a series bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV. 

Disclosed are compounds that are anandamide transport inhibitors and their pharmacological use.

Inhibitors of the anandamide transporter

Growing community of inventors

South Glastonbury, CT, United States of America

Chen Li